Statin (HMG-CoA reductase inhibitor)
HMG-CoA reductase inhibitor
- ↓ hepatic cholesterol synthesis at its rate-limiting step
- Upregulates hepatic LDL receptors → ↓ circulating LDL
- Myopathy and transaminase rise are the monitored class effects
- Blocks the rate-limiting step of cholesterol synthesis
- ➔ LDL reduction and cardiovascular risk reduction
- Myalgia; rarely rhabdomyolysis
- Interaction risk rises with CYP3A4 inhibitors
Drugs with this mechanism (7)
- Atorvastatin — The most-prescribed statin; potent LDL lowering.
- Fluvastatin — The 2C9-metabolized statin; useful when 3A4 interactions are the problem.
- Lovastatin — Food-dependent, CYP3A4-sensitive statin; now usually displaced by stronger, cleaner options.
- Pitavastatin — A statin with minimal CYP interactions.
- Pravastatin — A hydrophilic statin with few drug interactions.
- Rosuvastatin — The most potent statin for LDL lowering.
- Simvastatin — A widely used statin; many interactions, dose-limited by myopathy.
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